Synthesis Development of the Selective Estrogen Receptor Degrader (SERD) LSZ102 from a Suzuki Coupling to a C-H Activation Strategy was written by Baenziger, Markus;Baierl, Marcel;Devanathan, Krishnaswamy;Eswaran, Sumesh;Fu, Peng;Gschwend, Bjoern;Haller, Michael;Kasinathan, Gopu;Kovacic, Nikola;Langlois, Audrey;Li, Yongfeng;Schuerch, Friedrich;Shen, Xiaodong;Wan, Yinbo;Wickendick, Regina;Xie, Siwei;Zhang, Kai. And the article was included in Organic Process Research & Development in 2020.Application of 90560-10-4 This article mentions the following:
The development of the synthetic process to the selective estrogen receptor degrader (SERD) drug candidate LSZ102 from the medicinal chem. synthesis to the streamlined large-scale manufacturing route is described. The synthesis of LSZ102 could be significantly improved in regard to overall yield, removal of all chromatog. purifications, and reduction in the number of steps by revisiting the original disconnection strategy. Key features of the final process include construction of the benzothiophene core via Higa cyclization, late-stage phenolation using a Pd-catalyzed hydroxylation of an aryl bromide, and end-game assembly through a Pd-catalyzed C-H activation step. The overall yield could be significantly improved, and the costs could be reduced. In the experiment, the researchers used many compounds, for example, 6-Methoxybenzo[b]thiophene (cas: 90560-10-4Application of 90560-10-4).
6-Methoxybenzo[b]thiophene (cas: 90560-10-4) belongs to benzothiophene derivatives. Functionalized benzothiophenes are important constructs found in molecules with wide ranging biological activity and in organic materials. The different substitution patterns in these heterocycles offer new opportunities for drug discovery and other applications in materials science.Application of 90560-10-4
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem